1. PI3K/Akt/mTOR
  2. PI3K
  3. AS-252424

AS-252424 

Cat. No.: HY-13532 Purity: 97.52%
Handling Instructions

AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.

For research use only. We do not sell to patients.

AS-252424 Chemical Structure

AS-252424 Chemical Structure

CAS No. : 900515-16-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 101 In-stock
Estimated Time of Arrival: December 31
5 mg USD 92 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE AS-252424

    AS-252424 purchased from MCE. Usage Cited in: J Mol Med (Berl). 2018 Feb;96(2):119-133.

    The regulation of PHP14 on Akt phosphorylation is possibly via PI3Kγ in LX-2 cells. Cells are serum starvation 24 h, then treated TGF-β1 (10 ng/mL) 2 h, then added LY294002 (5 μM) or AS252424 (10 μM) as indicated; after another 2 h incubation, Western blot is performed to assess the protein expression of p-Akt.
    • Biological Activity

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    • References

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    Description

    AS-252424 is a potent and selective PI3Kγ inhibitor with an IC50 of 30±10 nM.

    IC50 & Target

    PI3Kγ

    30 nM (IC50)

    PI3Kα

    935 nM (IC50)

    PI3Kδ

    20 μM (IC50)

    PI3Kβ

    20 μM (IC50)

    In Vitro

    AS-252424 also inhibits PI3Kα, PI3Kβ and PI3Kδ with IC50s of 935±150 nM, 20 μM and 20 μM, respectively. AS-252424 inhibits MCP-1-mediated chemotaxis in wild-type primary monocytes in a concentration-dependent manner with an IC50 value of 52 μM, as well as in the monocytic cell line THP-1 with an IC50 value of 53 μM. In the human monocytic cell line THP-1, MCP-1 binding to the GPCR chemokine receptor CCR2, strongly induces phosphorylation of PKB/Akt, which is effectively inhibited by AS-252424 at IC50 values as low as 0.4 μM. In contrast, induction of PKB/Akt phosphorylation by colony stimulating factor (CSF-1), binding to the growth factor receptor c-fms, is only blocked by AS-252424 at IC50 values as high as 4.7 μM[1].

    In Vivo

    Oral administration of AS-252424 in a mouse model of acute peritonitis leads to a significant reduction of leukocyte recruitment. To evaluate the efficacy of AS-252424 to block leukocyte migration in vivo, it is tested in a mouse model of thioglycollate-induced peritonitis. Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%±14%), almost matching the result observed in PI3Kγ-deficient mice. Given the short oral half-life of AS-252424 (t1/2=1 h) and relative high clearance (2.25 L/kg per h), investigations at later time points (24-48 h) to assess macrophage and monoycyte recruitment are not undertaken. The modest pharmacokinetic properties do not appear to be caused by rapid oxidative metabolism (microsomal metabolism after 1 h: 16% (rat), 10% (human))[1].

    Molecular Weight

    305.28

    Formula

    C₁₄H₈FNO₄S

    CAS No.

    900515-16-4

    SMILES

    O=C(NC/1=O)SC1=C/C2=CC=C(C3=CC=C(F)C=C3O)O2

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 57 mg/mL (186.71 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2757 mL 16.3784 mL 32.7568 mL
    5 mM 0.6551 mL 3.2757 mL 6.5514 mL
    10 mM 0.3276 mL 1.6378 mL 3.2757 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    A PI3Kγ lipid kinase assay, based on the neomycin-coated scintillation proximity assay (SPA) bead technology, is performed in 384-well plates using ATP/[γ33P]ATP and PtdIns. Kinase assays for IC50 value determinations with PI3Kα, PI3Kβ, and PI3Kδ are carried out[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    After 3 h of starvation in serum-free medium, Raw-264 macrophages are pretreated with inhibitors (e.g., AS-252424, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM and 100 μM) or DMSO for 30 min and stimulated for 5 min with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Mice[1]
    PI3Kγ knockout (KO) mice are used. Oral administration of AS-252424 at 10 mg/kg is performed in PI3Kγ-deficient mice.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Product Name:
    AS-252424
    Cat. No.:
    HY-13532
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